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羟羧氧酰胺菌素的比较评估:抗菌活性、药代动力学、不良反应及临床疗效。

A comparative evaluation of moxalactam: antimicrobial activity, pharmacokinetics, adverse reactions, and clinical efficacy.

作者信息

Fitzpatrick B J, Standiford H C

出版信息

Pharmacotherapy. 1982 Jul-Aug;2(4):197-212. doi: 10.1002/j.1875-9114.1982.tb03187.x.

Abstract

Although moxalactam is not, technically speaking, a cephalosporin it is chemically and microbiologically so closely related to those compounds that it can be viewed as a member of the cephalosporin family. Moxalactam has a spectrum of activity that includes both gram positive and gram negative bacteria. Its gram positive activity is less than earlier cephalosporins, but its activity against the Enterobacteriaceae is similar to that of the aminoglycoside family of antibiotics in most comparative studies. Although moxalactam is considerably less active against gram positive bacteria than cefotaxime, another third generation cephalosporin, its higher and more prolonged serum levels probably offset this disadvantage. Compared to cefoperazone, the stability of moxalactam to many types of beta lactamases produced by gram negative bacteria may be advantageous in the therapy of infections caused by hospital-acquired pathogens. Clinical studies suggest that moxalactam can be used for empiric therapy of suspected gram negative infections when Pseudomonas and other non-fermentative bacteria, such as Acinetobacter, are not suspected. Impressive improvements in the survival of patients with gram negative enteric bacillary meningitis have been reported. Although moxalactam, cefotaxime, and cefoperazone have activity against Pseudomonas aeruginosa, none of these antibiotics should be used alone as therapy for suspected or proven severe systemic infections caused by this pathogen. Cost is a major problem with all of the new cephalosporin-like antibiotics. While this high cost may be partially balanced by the use of a single agent compared to an antibiotic combination for therapy in some situations, these antibiotics are not cost effective for prophylactic use. Superinfection with fungi, such as Candida, and Streptococcus faecalis have occurred, and toxicities, such as bleeding due to vitamin K deficiency and disulfuram-like reactions, have also been reported. Reports of resistance to moxalactam and the other third generation cephalosporins are of major concern and indicate the need to closely monitor antibiotic susceptibility patterns of hospital acquired organisms if these antibiotics are to be used for empiric therapy of suspected gram negative non-pseudomonas sepsis.

摘要

从技术层面讲,虽然拉氧头孢并非头孢菌素,但它在化学和微生物学方面与那些化合物密切相关,因此可被视为头孢菌素家族的一员。拉氧头孢的抗菌谱包括革兰氏阳性菌和革兰氏阴性菌。其对革兰氏阳性菌的活性低于早期的头孢菌素,但在大多数比较研究中,它对肠杆菌科细菌的活性与氨基糖苷类抗生素相似。虽然拉氧头孢对革兰氏阳性菌的活性远低于另一种第三代头孢菌素头孢噻肟,但其较高且持续时间更长的血清水平可能抵消了这一劣势。与头孢哌酮相比,拉氧头孢对革兰氏阴性菌产生的多种β-内酰胺酶的稳定性,在治疗医院获得性病原体引起的感染中可能具有优势。临床研究表明,当不怀疑有铜绿假单胞菌和其他非发酵菌(如不动杆菌)时,拉氧头孢可用于疑似革兰氏阴性感染的经验性治疗。据报道,革兰氏阴性肠道杆菌性脑膜炎患者的生存率有显著提高。虽然拉氧头孢、头孢噻肟和头孢哌酮对铜绿假单胞菌有活性,但这些抗生素都不应单独用于治疗由该病原体引起的疑似或确诊的严重全身感染。成本是所有新型头孢菌素类抗生素的一个主要问题。虽然在某些情况下,与联合使用抗生素治疗相比,使用单一药物可能会部分抵消这种高成本,但这些抗生素用于预防时并不具有成本效益。已发生念珠菌等真菌和粪肠球菌的二重感染,也有维生素K缺乏导致出血和双硫仑样反应等毒性反应的报道。对拉氧头孢和其他第三代头孢菌素耐药的报道令人高度关注,这表明如果要将这些抗生素用于疑似革兰氏阴性非铜绿假单胞菌败血症的经验性治疗,就需要密切监测医院获得性病原体的抗生素敏感性模式。

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